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Discovery of 2-aminoimidazopyridine adenosine A2A receptor antagonists

✍ Scribed by Brian F. McGuinness; Andrew G. Cole; Guizhen Dong; Marc-Raleigh Brescia; Yuefei Shao; Ian Henderson; Laura L. Rokosz; Tara M. Stauffer; Neelima Mannava; Earl F. Kimble; Catherine Hicks; Nicole White; Pamela G. Wines; Elizabeth Quadros

Book ID: 104004788
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 813 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.08.064

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✦ Synopsis

A novel series of adenosine A(2A) receptor antagonists was identified by high-throughput screening of an encoded combinatorial compound collection. The initial hits were optimized for A(2A) binding affinity, A(1) selectivity, and in vitro microsomal stability generating orally available 2-aminoimidazo[4,5-b]pyridine-based A(2A) antagonist leads.

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